华蟾酥毒基在大鼠胃肠道的吸收动力学  

Absorption Kinetics of Cinobufagin in Rat Gastrointestine

作　　者：徐莉[1] 孙星 林桂涛[1] 

机构地区：[1]山东中医药大学,济南250355 [2]迪沙药业集团有限公司,山东威海264205

出　　处：《中国实验方剂学杂志》2015年第1期102-106,共5页Chinese Journal of Experimental Traditional Medical Formulae

基　　金：济南市科技局高校自主创新项目(JN100586)

摘　　要：目的:研究华蟾酥毒基在大鼠胃、肠以及各肠段吸收动力学特征及吸收机制。为华蟾酥毒基的开发提供依据。方法:应用大鼠在体灌流技术,取低、中、高不同质量浓度(11,22,33 mg·L-1)华蟾酥毒基在大鼠胃、小肠中灌流3 h,以高效液相色谱法测定华蟾酥毒基的浓度,研究华蟾酥毒基大鼠胃肠道的吸收特征。结果:华蟾酥毒基低、中、高质量浓度在胃、小肠中灌流3 h均能较好的吸收,累积吸收量均为75%左右,且与药物的浓度无关,在小肠中的吸收表现出明显的一级动力学特征,3种浓度吸收速率常数分别为0.548,0.547,0.590 h-1;华蟾酥毒基在各肠段均能吸收,均呈一级动力学模式,十二指肠、空肠、回肠和结肠的吸收速率常数依次为0.024 6,0.015 2,0.016 4,0.013 5 cm-1·h-1。结论:华蟾酥毒基在大鼠胃、全肠道均能吸收;吸收呈一级动力学过程,吸收机制为被动扩散。Objective： To explore the absorption kinetics and absorption mechanisms of cinobufagin in the gastrointestine of rats, and to provide a basis for the development of cinohufagin. Method： The absorption kinetics were obtained by using the in situ perfusion method in rat. The concentration was determinated using HPLC method. Result： After 3 hours perfusion, cinobufagin in different concentrations （11, 22, 33 mg·L-1） can be better absorpted both in the stomach and small intestine, and the cumulative uptake was 75%. The absorption kinetics were independent of the concentration of the drug. Absorption in the small intestine showed obvious first- order kinetics characteristics, and absorption rate constant of three concentrations was 0. 548, 0. 547, 0. 590 h -1 , respectively. Cinobufagin was absorbed in all segments of intestine, and it showed a first-order process with passive diffusion mechanism. The absorption rate constant in the duodenum, jejunum, ileum, and colon were 0. 024 6, 0. 015 2, 0. 016 4, 0. 013 5 cm-1·h-1 , respectively. Conclusion： Cinobufagin was absorbed in the stomach and all segments of intestine of rats, and its absorption kinetics was a first-order process with passive diffusion mechanism.

关 键 词：华蟾酥毒基 吸收动力学 高效液相色谱法 在体胃肠吸收 

分 类 号：R285.5[医药卫生—中药学]